225Ac-FAP-2286

225Ac-FAP-2286 is an investigational peptide-targeted radionuclide therapy (PTRT) consisting of the fibroblast activation protein (FAP)-binding peptide FAP-2286 labeled with the alpha-emitting radioisotope actinium-225 (225Ac). FAP is a cell-surface glycoprotein highly expressed on cancer-associated fibroblasts (CAFs) within the stroma of most epithelial tumors, as well as on certain mesenchymal tumor cells, while showing limited expression in normal adult tissues. By targeting FAP, 225Ac-FAP-2286 delivers potent alpha radiation directly to the tumor microenvironment. Alpha particles possess high linear energy transfer, causing complex double-stranded DNA breaks that are difficult for cells to repair, leading to cell death. Originally developed by Clovis Oncology in partnership with Evergreen Theragnostics, the FAP-2286 program was later acquired by Novartis. It is currently being investigated for the treatment of various advanced solid tumors, including pancreatic, head and neck, and colorectal cancers.

Other names

Actinium-225 FAP-2286Actinium225 FAP-2286Actinium 225 FAP-2286[225Ac]-FAP-2286225Ac-labeled FAP-2286